[1]. Lee SJ, et al. Mechanism of inhibition by chlorpromazine of the human pain threshold sodium channel, Nav1.7. Neurosci Lett. 2017 Feb 3;639:1-7
[2]. Kale OE, et al. Amlodipine, an L-type calcium channel blocker, protects against chlorpromazine-induced neurobehavioural deficits in mice. Fundam Clin Pharmacol. 2017 Jan 19
[3]. Sampaio LR, et al. Electroencephalographic study of chlorpromazine alone or combined with alpha-lipoic acid in a model of schizophrenia induced by ketamine in rats. J Psychiatr Res. 2017 Mar;86:73-82
[4]. Suzuki H, et al. Comparison of the anti-dopamine D? and anti-serotonin 5-HT(2A) activities of chlorpromazine, bromperidol, haloperidol and second-generation antipsychotics parent compounds and metabolites thereof. J Psychopharmacol. 2013 Apr;27(4):396-400
[5]. Thomas, D., et al. The antipsychotic drug chlorpromazine inhibits HERG potassium channels. Br J Pharmacol, 2003. 139(3): p. 567-74.
规格
10mg 50mg
是D2,5HT2A,钾通道和钠通道的拮抗剂。也是一种细胞内吞抑制剂。
使用本产品的应用案例(仅供参考)
In Vitro
Cell(HepG2), 20 µg/mL, 1 h, 37°C
For initial study of cellular internalization, NPs-EPI was incubated with tumor spheroids at an EPI concentration of 8 µg/mL for 4 h. The tumor spheroids were grown as our previous reported procedure. Briefly, HepG2 cells were seeded in 96-well plates at a density of 8×103 per well precoated with 50 µL of 1% low melting point agarose. Cells were cultured to obtain multicellular spheroids (400–500 μm in diameter) for subsequent studies. After incubation with NPs-EPI, tumor spheroids were rinsed three times with cold PBS and processed for image analysis by TEM.
To investigate the internalization pathways of NPs-EPI, HepG2 cells were seeded into 6-well plates with 2×105 cells per well and incubated for 24 hours. The cells were then pre-treated with different endocytic inhibitors (chlorpromazine hydrochloride 20 µg/mL, amiloride hydrochloride 200 µg/mL) at 37°C for 1 hour. Subsequently, NPs-EPI (EPI 8 µg/mL) were added and incubated at 37°C for 2 hours. Finally, the cells were washed three times with cold PBS and harvested for flow cytometry to determine the fluorescence intensity of EPI (Ex=488, Em=588). Cells pre-treated with PBS at 37°C served as the positive control group. Internalization assays were also performed in the absence of endocytic inhibitors at 4°C when indicated.
来源文献:Chen E, Han S, Song B, Xu L, Yuan H, Liang M, Sun Y. Mechanism Investigation of Hyaluronidase-Combined Multistage Nanoparticles for Solid Tumor Penetration and Antitumor Effect. Int J Nanomedicine. 2020 Aug 24;15:6311-6324. doi: 10.2147/IJN.S257164. PMID: 32922003; PMCID: PMC7458542.
Cell ,100 μM,30 min
To investigate the endocytosis mechanism involved in the uptake process, cells were pre-treated with endocytic inhibitors including chlorpromazine (100 μM), genistein (200 μM), and amiloride (200 µM) for 30 min. Ten the cells were treated with 1 μg of FITC-labeled DMSNs for 6 h. In a control group, cells were not treated with the inhibitors prior to nanoparticle treatment. Cellular uptakes of nanoparticles were quantitated by fow cytometer as described above.
来源文献:Mo C, Lu L, Liu D, Wei K. Development of erianin-loaded dendritic mesoporous silica nanospheres with pro-apoptotic effects and enhanced topical delivery. J Nanobiotechnology. 2020 Mar 30;18(1):55. doi: 10.1186/s12951-020-00608-3. PMID: 32228604; PMCID: PMC7104482.